4.5 Article

4-aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 16, Issue 6, Pages 1502-1505

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.12.053

Keywords

cathepsin K inhibitors; osteoporosis; 3-biphenylamino acid amides; 4-aminophenoxyacetic acids

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We have designed and synthesized a novel series of 3-biphenylamino acid amides as cathepsin K inhibitors based on compound I. in these inhibitors, we have discovered 4-aminophenoxyacetic acids 43 and 47 with good IC50 values, although lipophilic groups are favorable for the hydrophobic S1' pocket. (C) 2005 Elsevier Ltd. All rights reserved.

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